*  Stablon is a smart drug - BrainMeta.com Forum
Agomelatine works as an antagonist on the serotonin 5-HT2C receptor whereas Stablon it's 'unknown', here is what wikipedia says ... Tianeptine stimulates the opioid receptors and when coming off of it after an extended period will put you in painful withdrawl ... Tianeptine, indicated as a thymoleptic, reduces the effects of serotonin in the limbic system and the pre-frontal cortex. With ... Tianeptine stimulates the opioid receptors and when coming off of it after an extended period will put you in painful withdrawl ...
  http://brainmeta.com/forum/index.php?showtopic=14231&st=330
*  Desmetramadol - Wikipedia
Desmetramadol is also an antagonist of the serotonin 5-HT2C receptor, at pharmacologically relevant concentrations. ... While the multiple receptor targets can be beneficial in the treatment of pain (especially complex pain syndromes such as ... It also shows comparatively far lower affinity for the δ- and κ-opioid receptors. The two enantiomers of desmetramadol show ... on serotonin (5-HT) efflux and uptake in the rat dorsal raphe nucleus". Br J Anaesth. 79 (3): 352-6. doi:10.1093/bja/79.3.352. ...
  https://en.wikipedia.org/wiki/Desmetramadol
*  5-HT(2C) antagonism blocks blood oxygen level-dependent pharmacological-challenge magnetic resonance imaging signal in rat...
... receptor antagonists, SB 224289 (2.5 mg/kg) and SB 242084 (2 mg/kg), respectively. Subcutaneous injection of mCPP (3 mg/kg) ... pharmacological-challenge magnetic resonance imaging was used to further characterize the central action of serotonin on ... receptor antagonist but was partially reversed by the 5-HT(2C) receptor antagonist. mCPP alone induced both positive and ... antagonist SB 242084 reversed the effects elicited by mCPP, whereas the 5-HT(1B) antagonist SB 224289 had virtually no impact. ...
  https://www.ndcn.ox.ac.uk/publications/106546
*  6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide - Wikipedia
... is a drug which acts as a potent and selective antagonist for the serotonin 5-HT2C receptor. In animal studies it was found to ... receptor antagonist potentiates a low dose amphetamine-induced conditioned place preference. Neuroscience Letters. 2011 Nov 7; ... 6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide (CEPC) ... demonstrating that 5-HT2C-mediated disinhibition of dopamine ...
  https://en.wikipedia.org/wiki/6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide
*  Nefazodone - Wikipedia
It has been described as a serotonin antagonist and reuptake inhibitor (SARI) due to its combined actions as a potent serotonin ... It also has high affinity for the α1-adrenergic receptor and serotonin 5-HT1A receptor, and relatively lower affinity for the ... Nefazodone acts primarily as a potent antagonist of the serotonin 5-HT2A receptor and to a lesser extent of the serotonin 5- ... HT2C receptor. ... Millan MJ (2005). "Serotonin 5-HT2C receptors as a target for ...
  https://en.wikipedia.org/wiki/Nefazodone
*  SuperBiHelix method for predicting the pleiotropic ensemble of G-protein-coupled receptor conformations | PNAS
2011) Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors. J Chem Inf ... the histamine H3 receptor (26), the CCR5 receptor (27, 28), TAS2R38 bitter taste receptor (29), and the V2 vasopressin receptor ... 2008) The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science 322(5905):1211-1217. ... 2011) Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor. Proteins 79(6):1878-1897. ...
  http://www.pnas.org/content/111/1/E72
*  RS-102221 - Wikipedia
... which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT2C receptor ... receptors potentiates consequences of serotonin reuptake blockade. Neuropsychopharmacology. 2004 Oct;29(10):1782-9. PMID ... Serotonin 5-HT(2C) receptors in nucleus accumbens regulate expression of the hyperlocomotive and discriminative stimulus ... PMID 12721337 Morita K, Hamamoto M, Arai S, Kitayama S, Irifune M, Kawahara M, Kihira K, Dohi T. Inhibition of serotonin ...
  https://en.wikipedia.org/wiki/RS-102221
*  ChemiScreen™ Human Recombinant 5-HT 2C Serotonin Receptor Calcium-Optimized Stable Cell Line from MilliporeSigma |...
Human Recombinant 5-HT 2C Serotonin Receptor Calcium-Optimized Stable Cell Line from MilliporeSigma on SelectScience ... Thus, the cell line is an ideal tool for screening for antagonists of interactions between 5-HT2C and its ligands. ... Thus, the cell line is an ideal tool for screening for antagonists of interactions between 5-HT2C and its ligands. ... Chemicon's cloned human 5-HT2C -expressing cell line is made in the Chem-1 host, which supports high levels of recombinant 5-HT ...
  http://www.selectscience.net/products/chemiscreen--human-recombinant-5-ht-2c--serotonin-receptor-calcium-optimized-stable-cell-line/?prodID=106481&u=F498D1B4-7F21-4F88-89D3-5B1D3DA1B088&techBID=50
*  TIK-301 - Wikipedia
It also acts as an antagonist at serotonin receptors 5-HT2B and 5-HT2C. TIK-301 is administered orally. Compared to melatonin, ... Because of its affinity for serotonin receptors, it has potential to serve as a possible antidepressant drug, similar to ... "Recent progress in the development of agonists and antagonists for melatonin receptors". Current medicinal chemistry. 19 (21): ... Because of its receptor specific action, there are no associated changes in core body temperatures, heart rate or blood ...
  https://en.wikipedia.org/wiki/TIK-301
*  A new chronobiological approach to discriminate between acute and chronic depression using peripheral temperature, rest...
One study using an agonist at MT(1)/MT(2) melatonin receptors and an antagonist at 5-HT(2C) serotonin receptors showed a ... serotonin) receptor 2C. HAM-D: Hamilton Depression Scale. HCPA: Hospital de Clínicas de Porto Alegre ... Figure 5 Mean levels of peripheral temperature (diurnal and nocturnal) expressed as a function of activity level (expressed as ... In the day and at night, peripheral temperature decreased as activity increased (Figure 5). However, for the same level of ...
  https://bmcpsychiatry.biomedcentral.com/articles/10.1186/1471-244X-13-77
*  5-HT2C receptor agonist - Wikipedia
In the late 1960s, non-selective serotonin receptor antagonists demonstrated a relationship between serotonin receptors and ... Later, animal studies showed that serotonin receptor agonists might act as a mediator of satiety. Serotonin has been implicated ... "The structure of human serotonin 2c G-protein-coupled receptor bound to agonists and antagonists". Journal of Molecular ... When serotonin binds to the receptors, the most important contacts are in TM helixes 3, 5 and 6 (Figure 3), while the other ...
  https://en.wikipedia.org/wiki/5-HT2C_receptor_agonist
*  5-HT2C receptor - Wikipedia
... a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, ... It is the only serotonin receptor as well as the only member of the large family of 7 transmembrane receptors (7TMRs) known to ... "Serotonin activates the hypothalamic-pituitary-adrenal axis via serotonin 2C receptor stimulation". The Journal of Neuroscience ... Activation of this receptor by serotonin inhibits dopamine and norepinephrine release in certain areas of the brain. 5-HT2C ...
  https://en.wikipedia.org/wiki/5-HT2C_receptor
*  2C-H - Wikipedia
It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat stomachs. It exhibits binding ... It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ... It exhibits agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with ... 2C-H, or 2,5-dimethoxyphenethylamine, is a lesser-known substituted phenethylamine of the 2C family. 2C-H was first synthesized ...
  https://en.wikipedia.org/wiki/2C-H
*  SB-206553 - Wikipedia
Canal CE; Olaghere da Silva UB; Gresch PJ; Watt EE; Sanders-Bush E; Airey DC (April 2010). "The serotonin 2C receptor potently ... receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)". The Journal ... receptor antagonists". Journal of Medicinal Chemistry. 39 (25): 4966-77. doi:10.1021/jm960571v. PMID 8960557. Bromidge SM; ... "Selective blockade of serotonin-2C/2B receptors enhances mesolimbic and mesostriatal dopaminergic function: a combined in vivo ...
  https://en.wikipedia.org/wiki/SB-206553
*  Teenage Violence
The relations of these receptors to pain and aggression are very complex. At the level of the spinal cord, serotonin inhibits ... The antidepressants nefazodone, trazodone, and mirtazapine are antagonists at 5-HT2A, but do no appear to have antipsychotic ... There are at least 15 subtypes of serotonin receptors in the brain that serve different functions in different locations. ... The benefit that results from increased serotonergic tone involves down-regulation of receptors and decreased receptor ...
  http://goertzel.org/dynapsyc/1998/TeenageViolence.html
*  Bone Resorption
... receptors, and acts as an antagonist at this receptor subtype 63 . Agomelatine has shown antidepressant activity... ... for human cloned serotonin-2C (5-HT2C) ... P2X7 receptor antagonists. *Peptide Bradykinin B2 Receptor ... Agomelatine 7 is a potent agonist at melatoninergic receptors. It shows a high affinity for cloned human melatonin receptor MT1 ... A major complication associated with C5a antagonists arises from the fact that historically, most C5a receptor active ligands ...
  https://www.americorpshealth.biz/bone-resorption/
*  Amesergide - Wikipedia
Amesergide (INN, USAN; developmental code name LY-237733) is a serotonin receptor antagonist of the ergoline and lysergamide ... Leopoldo M (2004). "Serotonin(7) receptors (5-HT(7)Rs) and their ligands". Curr. Med. Chem. 11 (5): 629-61. PMID 15032609. Marc ... Amesergide acts as a selective antagonist of the serotonin 5-HT2A, 5-HT2B, 5-HT2C receptors (Ki = 1.96-15.1 nM). It is also an ... The drug is a potent antagonist of the α2-adrenergic receptor in addition to the 5-HT2 receptors via its major active ...
  https://en.wikipedia.org/wiki/Amesergide
*  Halogenated Indole Alkaloids from Marine Invertebrates
They have also been found to modulate serotonin receptors [39].. Aplysinopsin-type compounds have been reported from multiple ... antagonist binding from cloned human serotonin 5-HT2C receptors expressed in a mammalian cell line (Ki = 2.3 μM and Ki = 0.33 ... compared with serotonin affinity values Ki = 0.32 μM at the 5-HT2A receptor and Ki = 0.13 μM at the 5-HT2C receptor [46]. ... in the binding to human serotonin 5-HT2 receptors. The length of the alkyl chain at the R3 position as well as the bromination ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC2885079/
*  5-HT2A receptor - Wikipedia
Serotonin): Receptor Agonists and Antagonists". In Brunton LL, Lazo JS, Parker K. Goodman & Gilman's the Pharmacological Basis ... Serotonin receptors were split into two classes by Gaddum and Picarelli when it was discovered that some of the serotonin- ... Feng J, Cai X, Zhao J, Yan Z (September 2001). "Serotonin receptors modulate GABA(A) receptor channels through activation of ... as well as an antagonist on other serotonin receptors. Mirtazapine is a 5-HT2A, 5-HT2C, and 5-HT3 antagonist. Mirtazapine also ...
  https://en.wikipedia.org/wiki/5-HT2A_receptor
*  Mirtazapine - Wikipedia
The drug acts as an antagonist of certain adrenergic and serotonin receptors, and is also a strong antihistamine. It is ... It is specifically a potent antagonist or inverse agonist of the α2A-, α2B-, and α2C-adrenergic receptors, the serotonin 5-HT2A ... This is in accordance with the fact that it is not a serotonin reuptake inhibitor or MAOI, nor a serotonin receptor agonist. ... As an H1 receptor antagonist, mirtazapine is extremely potent, and is in fact the most potent of all the TCAs and TeCAs. ...
  https://en.wikipedia.org/wiki/Mirtazapine
*  Doxepin - Wikipedia
It is specifically an antagonist of the histamine H1 and H2 receptors, the serotonin 5-HT2A and 5-HT2C receptors, the α1- ... and similarly has no effect on other receptors such as adrenergic and serotonin receptors. The H1 receptor antagonism of ... Although doxepin is selective for the H1 receptor at doses lower than 25 mg, blockade of serotonin and adrenergic receptors may ... In fact, doxepin has been said to be the most or one of the most potent H1 receptor antagonists available, with one study ...
  https://en.wikipedia.org/wiki/Doxepin
*  SDZ SER-082 - Wikipedia
... with good selectivity over other serotonin receptor subtypes and slight preference for 5-HT2C over 5-HT2B. It has been used in ... SDZ SER-082 is a drug which acts as a mixed antagonist for the 5-HT2B and 5-HT2C serotonin receptors, ... Filip M (2005). "Role of serotonin (5-HT)2 receptors in cocaine self-administration and seeking behavior in rats". ... Filip M, Bubar MJ, Cunningham KA (January 2006). "Contribution of serotonin (5-HT) 5-HT2 receptor subtypes to the ...
  https://en.wikipedia.org/wiki/SDZ_SER-082
*  α<sub>2C</sub>-adrenoceptor | Adrenoceptors | IUPHAR/BPS Guide to...
Mirtazapine is an antagonist of α2-adrenoceptors and serotonin 5-HT2a and 5-HT2c receptors.. ... 1994) Expression of α2-adrenergic receptor genes in rat tissues. Receptor, 4: 191-199. [PMID:7812219] ... α2-C4 , ADRA2L2 , ADRA2RL2 , Adrenergic alpha2C- receptor class I , alpha-2 adrenergic receptor subtype C4 , alpha-2C ... 1988) Cloning and expression of a human kidney cDNA for an α2- adrenergic receptor subtype. Proc. Natl. Acad. Sci. U.S.A., 85: ...
  http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=27
*  Amitriptyline - Wikipedia
... and as an agonist of the sigma σ1 receptor. It has also been shown to be a relatively weak NMDA receptor antagonist via the ... Amitriptyline additionally acts as an antagonist or inverse agonist of the serotonin 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 ... receptors, the α1-adrenergic receptor, the histamine H1 and H2 receptors, and the muscarinic acetylcholine receptors, ... Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (1993). "Cloning and expression of a novel serotonin receptor with high ...
  https://en.wikipedia.org/wiki/Amitriptyline
*  Medifoxamine - Wikipedia
Martin P, Lemonnier F (1994). "[The role of type 2 serotonin receptors, 5-HT2A and 5-HT2C, in depressive disorders: effect of ... but also as an even weaker serotonin reuptake inhibitor (IC50 = 1,500 nM) and as a weak antagonist of the 5-HT2A and 5-HT2C ... Medifoxamine and its metabolites lack affinity for other serotonin receptors including 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT3 (> ... very low affinity for the muscarinic acetylcholine receptors and 10-fold lower affinity for the α1-adrenergic receptor relative ...
  https://en.wikipedia.org/wiki/Medifoxamine